Mucoadhesive thermoresponsive medicament-carrier composition

a thermoresponsive, medicament-carrier technology, applied in the direction of fluorescence/phosphorescence, inorganic non-active ingredients, peptide/protein ingredients, etc., can solve the problems of undesired side effects, kill tumor cells, damage and death of cells, etc., and achieve good drug delivery effect and little side effects

Inactive Publication Date: 2007-10-04
PHARMA POWER BIOTEC
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Benefits of technology

[0001] The object of this invention is to prepare a medicament-carrier composition for the convenience of use, which has good drug delivery effect and little side effect, and which mainly comprises a mucoadhesive polymer and a thermoresponsive polymer. The medicament-carrier composition according to this invention is quite suitable for use in topical delivery of biological active compounds, especially those useful in photodynamic diagnosis or therapy, e.g. 5-aminolevulinic acid (abbreviated to “ALA”).

Problems solved by technology

The photosensitive agents are generally inert, and they will stimulate the production of toxic substances to cause the damage and death of cells, and finally kill the tumor cells when they are exposed to the radiation of certain wavelengths.
Most of ALA solution applied flows to gastrointestinal tract and is absorbed and distributed over the body, thereby resulting in undesired side effects.
As it should be formulated before use and should be used immediately after formulation, it is not practical. V. Vonoxa et al (J. Pharm. Pharmacol. 1997, 49: 652-656 “Potential efficacy of a delta 5-ALA bioadhesive gel formulation for the PDT of lesions of the GI tract in mice) attempted to formulate ALA in a bioadhesive gel having uniform composition.
However, it is found that some side effects associated with the gastrointestinal tract such as nausea and vomit occured during these treatments depend on the dose of ALA (Stummer et al, “Intraoperative detection of malignant fluorescence”, Neurosurgery 1998; 42:518-525).
In view of the drug delivery systems for topical use disclosed in this art, the usage form, convenience and drug delivery effect are still unsatisfactory.

Method used

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  • Mucoadhesive thermoresponsive medicament-carrier composition
  • Mucoadhesive thermoresponsive medicament-carrier composition
  • Mucoadhesive thermoresponsive medicament-carrier composition

Examples

Experimental program
Comparison scheme
Effect test

example 1.1

[0063] Pluronic F-127 (PF-127) is a polymer having revserse thermal gelation. The early reports of Achmolka (Schmolka I R. Artificial skin. I. “Preparation and properties of pluronic F-127 gels for treatment of burns”, Journal of Biomedical Materials Research. 6(6):571-82, 1972) and the current results of other researchers (1. Morishita M. Barichello J M. Takayama K. Chiba Y. Tokiwa S. Nagai T., “Pluronic F-127 gels incorporating highly purified unsaturated fatty acids for buccal delivery of insulin”, International Journal of Pharmaceutics. 212(2):289-93, 2001; 2. El-Kattan A F. Asbill C S. Kim N. Michniak B B., “Effect of formulation variables on the percutaneous permeation of ketoprofen from gel formations”, Drug Delivery: Journal of Delivery & Targeting of Therapeutic Agents 7(3):147-53, 2000; 3. Onuki Y. Morishita M. Takayama K. Tokiwa S. Chiba Y. Isowa K. Nagai T., “In vivo effects of highly purfied docosahexaenoic acid on rectal insulin absorption”, International Journal of Ph...

example 1.2

[0065] The sample and operation condition are as described in example 1.1 except that the specified amount of sample was cooled from 90° C. at a rate of 2° C. / min at a fixed volume and controlled temperature and at a speed of 400 rpm. The temperatures at which the rotor stoped (T2) and started revolution again (T1) were recorded, and the operation was stopped when the temperature was decreased to 4° C. The PF-127 was prepared into five concentration 10% w / w, 17.5% w / w, 20% w / w, 22.5% w / w, and 25% w / w. According to the procedure, the process was repeated three times to take the average, the results are shown in the Table 2 and FIG. 2.

TABLE 2PF-127 conc.(%, w / w)1st critical point(° C.)2nd critical point(° C.)10281317.560.4734.32062.9326.3322.573.23242570.723.67

example 1.3

[0066] The sample and operation condition are as described in example 1.1 and example 1.2. The square represents the result of temperature increase test and triangle represents the result of temperature decrease test. The concentration of PF-127 was fixed at 25% w / w. Various concentrations of Carbopol 971P were added. Repeat the process three times and take the average. The results of the tests are shown in the Table 3 and FIG. 3.

TABLE 325% w / wPF-127 +Carbopol2nd crictical2nd crictical1st crictical1st crictical971P ofpoint in thepoint in thepoint in thepoint in theconc. (%temp.temp.temp.temp.w / w)increase testdecrease testincrease testdecrease test070.769.1323.6721.430.560.758.6731.1325.170.854.8354.3333.232.37154.253.2334.734.871.251.3740.432.7338.87

[0067] The test results have shown that the addition of mucoadhesive polymer Carbopol 971P will not affect the first critical point and second critical point of thermoresponsive polymer PF-127 significantly. Therefore, this is an excel...

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Abstract

This invention relates to a medicament-carrier composition for use in delivering medicaments or fixing the action site of biological active compounds, which mainly comprises a mucoadhesive polymer and a thermoresponsive polymer. The medicament-carrier composition according to this invention is quite suitable for use in topically delivering biological active compounds, especially those useful in photodynamic diagnosis or therapy, e.g. 5-aminolevulinic acid (called as “ALA” for short).

Description

OBJECT OF THE INVENTION [0001] The object of this invention is to prepare a medicament-carrier composition for the convenience of use, which has good drug delivery effect and little side effect, and which mainly comprises a mucoadhesive polymer and a thermoresponsive polymer. The medicament-carrier composition according to this invention is quite suitable for use in topical delivery of biological active compounds, especially those useful in photodynamic diagnosis or therapy, e.g. 5-aminolevulinic acid (abbreviated to “ALA”). BACKGROUND OF THE INVENTION [0002] The final object of treating or diagnosing diseases with chemical medicaments is to deliver a suitable concentration of the drug molecules or the derivatives thereof to the site of subjects to be effected to achieve the diagnostic or therapeutic benefit while avoiding the occurrence of undesired side effect. This is especially desired for the patients afflicted with topical diseases such as skin cancer, oral cancer, tumor of la...

Claims

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Application Information

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Patent Type & Authority Applications(United States)
IPC IPC(8): A61K9/00G01N21/64A61K9/70A61K31/195A61K31/197A61K31/22A61K41/00A61K47/02A61K47/10A61K47/32A61K47/34A61K47/38A61K49/00A61P35/00
CPCA61K9/0043A61K9/006A61K9/7015A61K31/195A61K41/0061A61K47/32A61K47/34A61K47/38A61K49/0021A61K47/10A61P35/00
Inventor TSAI, TSUI-MIN
Owner PHARMA POWER BIOTEC
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